SR 1001 is a retinoic acid receptor-related orphan receptor (ROR) α and γ inverse agonist (Ki values are 172 and 111 nM respectively). SR1001 demonstrates no activity at RORβ or LXR. SR1001 suppresses Th17 cell differentiation and cytokine expression and reduces the severity of disease in an animal model of mulitple sclerosis.
Basic Clin Pharmacol Toxicol. 2021 Nov;129(5):357-368.
RORγt inhibitor SR1001 alleviates acute pancreatitis by suppressing pancreatic IL‐17‐producing Th17 and γδ‐T cells in mice with ceruletide‐induced pancreatitis
SR 1001 purchased from AbMole
| Molecular Weight | 477.4 |
| Formula | C15H13F6N3O4S2 |
| CAS Number | 1335106-03-0 |
| Solubility (25°C) | DMSO 41 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related ROR Products |
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| JTE-151
JTE-151 is a RORγ inhibitor that suppresses overactive immune responses by inhibiting RORγ associated with Th17 cell activation.JTE-151 can be used in studies related to autoimmune diseases. |
| SAR-441169
SAR-441169 is a RORγt inverse agonist that can be used in studies related to psoriasis. |
| GRC-39815
GRC-39815 is a RORγt inverse agonist that can be used in studies related to chronic obstructive pulmonary disease. |
| RORγ antagonist 1
RORγ antagonist 1, a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). |
| RORγt inverse agonist 31
RORγt inverse agonist 31 (14g) is a potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 0.428 μM. |
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